Rizact

Rizact Uses, Dosage, Side Effects, Food Interaction and all others data.

Rizact binds with high affinity to human cloned 5-HT1B/1D receptors. Rizact Benzoate presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system.

Rizact is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Rizact also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Rizact in humans.

Trade Name Rizact
Availability Prescription only
Generic Rizatriptan
Rizatriptan Other Names Risatriptan, Rizatriptán, Rizatriptan, Rizatriptanum
Related Drugs Ubrelvy, Botox, diclofenac, celecoxib, metoclopramide, sumatriptan, Imitrex, Reglan
Type Tablet
Formula C15H19N5
Weight Average: 269.3449
Monoisotopic: 269.164045633
Protein binding

14%

Groups Approved
Therapeutic Class 5-HT Agonists
Manufacturer Cipla Limited
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Rizact
Rizact

Uses

Rizact Benzoate is used for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years old.

Rizact is also used to associated treatment for these conditions: Migraine with acute onset aura, Acute Migraine without aura

How Rizact works

Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.

Dosage

Rizact dosage

Dosing Information In Adults: The recommended starting dose of Rizact Benzoate is either 5 mg or 10 mg for the acute treatment of migraines in adults. The 10-mg dose may provide a greater effect than the 5-mg dose, but may have a greater risk of adverse reactions.

Redosing In Adults: Although the effectiveness of a second dose or subsequent doses has not been established in placebocontrolled trials, if the migraine headache returns, a second dose may be administered 2 hours after the first dose. The maximum daily dose should not exceed 30 mg in any 24-hour period. The safety of treating, on average, more than four headaches in a 30-day period has not been established.

Dosing Information In Pediatric Patients (Age 6 to 17 Years): Dosing in pediatric patients is based on the patient's body weight. The recommended dose of Rizact Benzoate is 5 mg in patients weighing less than 40 kg, and 10 mg in patients weighing 40 kg or more.

The efficacy and safety of treatment with more than one dose of Rizact Benzoate within 24 hours in pediatric patients 6 to 17 years of age have not been established.

Dosage Adjustment For Patients On Propranolol: Sections or subsections omitted from the full prescribing information are not listed.

  • Adult Patients: In adult patients taking propranolol, only the 5-mg dose of Rizact Benzoate is recommended, up to a maximum of 3 doses in any 24-hour period (15 mg)
  • Pediatric Patients: For pediatric patients weighing 40 kg or more, taking propranolol, only a single 5-mg dose of Rizact Benzoate is recommended (maximum dose of 5 mg in a 24-hour period). Rizact Benzoate should not be prescribed to propranolol-treated pediatric patients who weigh less than 40 kg

Administration of Rizact Benzoate Tablets, administration with liquid is not necessary. Orally disintegrating tablets are packaged in a blister within an outer aluminum pouch and patients should not remove the blister from the outer pouch until just prior to dosing. The blister pack should then be peeled open with dry hands and the orally disintegrating tablet placed on the tongue, where it will dissolve and be swallowed with the saliva.

Side Effects

The following adverse reactions are discussed in more detail in other sections of the labeling:

  • Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina
  • Arrhythmias
  • Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure
  • Cerebrovascular Events
  • Other Vasospasm Reactions
  • Medication Overuse Headache
  • Serotonin Syndrome
  • Increase in Blood Pressure

Toxicity

Symptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.

Precaution

Elderly; mild to moderate hepatic or renal impairment; coronary artery disease; pregnancy, lactation. May cause drowsiness. History of seizures. Ensure an interval of at least 24 hr after stopping an ergotamine compound and starting a serotonin (5-HT1) agonist.

Interaction

Propranolol: The dose of Rizact should be adjusted in propranolol-treated patients, as propranolol has been shown to increase the plasma AUC of rizatriptan by 70%

Ergot-Containing Drugs: Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and Rizact within 24 hours is contraindicated

Other 5-HT1 Agonists: Because their vasospastic effects may be additive, co-administration of Rizact and other 5-HT1 agonists within 24 hours of each other is contraindicated

SSRIs /SNRIs And Serotonin Syndrome: Cases of serotonin syndrome have been reported during co-administration of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs)

Monoamine Oxidase Inhibitors: Rizact is contraindicated in patients taking MAO-A inhibitors and non-selective MAO inhibitors. A specific MAO-A inhibitor increased the systemic exposure of rizatriptan and its metabolite

Food Interaction

  • Take with or without food. However, the onset of action may be delayed by approximately 1 hour when taken with food.

Rizact Cholesterol interaction

[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.

Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).

Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.

In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.

As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.

Periodic cardiovascular evaluations should be performed during intermittent, long-term use.

Volume of Distribution

  • 140 L [male]
  • 110 L [female]

Elimination Route

Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.

Half Life

2-3 hours

Elimination Route

Approximately 14% of an oral dose is excreted in urine as unchanged rizatriptan while 51% is excreted as indole acetic acid metabolite, indicating substantial first pass metabolism.

Pregnancy & Breastfeeding use

Pregnancy: Inform patients that Rizact Benzoate should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Rizact Benzoate is administered to a nursing woman. Rizact is extensively excreted in rat milk, with levels in milk at least 5-fold higher than levels in maternal plasma.

Contraindication

Rizact Benzoate is contraindicated in patients with:

  • Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or other significant underlying cardiovascular disease
  • Coronary artery vasospasm including Prinzmetal's angina
  • History of stroke or transient ischemic attack (TIA)
  • Peripheral vascular disease (PVD)
  • Ischemic bowel disease
  • Uncontrolled hypertension
  • Recent use (i.e., within 24 hours) of another 5-HT1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide)
  • Hemiplegic or basilar migraine
  • Concurrent administration or recent discontinuation (i.e., within 2 weeks) of a MAO-A inhibitor
  • Hypersensitivity to Rizact Benzoate (angioedema and anaphylaxisseen)

Special Warning

Pediatric Use: Safety and effectiveness in pediatric patients under 6 years of age have not been established. The efficacy and safety of Rizact in the acute treatment of migraine in patients aged 6 to 17 years was established in an adequate and well-controlled study. The incidence of adverse reactions reported for pediatric patients in the acute clinical trial was similar in patients who received Rizact to those who received placebo. The adverse reaction pattern in pediatric patients is expected to be similar to that in adults.

Geriatric Use: Clinical studies of Rizact did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Although the pharmacokinetics of rizatriptan were similar in elderly (aged ≥65 years) and in younger adults (n=17), in general, dose selection for an elderly patient should be cautious, starting at the low end of the dosing range. This reflects the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Geriatric patients who have other cardiovascular risk factors (e.g., diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) should have a cardiovascular evaluation prior to receiving Rizact

Renal Impairment: For mild-moderate impairment, initate with 5 mg. Further dose of 5 mg may be taken after an interval of at least 2 hr. Max: 10 mg/24 hr. Avoid in severe impairment.

Hepatic Impairment: For mild-moderate impairment, initate with 5 mg. Further dose of 5 mg may be taken after an interval of at least 2 hr. Max: 10 mg/24 hr. Avoid in severe impairment.

Acute Overdose

May cause hypertension and CV symptoms. Gastric lavage using activated charcoal may be considered. Monitor ECG and clinical status of the patient.

Storage Condition

Store at 15-30° C.

Innovators Monograph

You find simplified version here Rizact

Rizact contains Rizatriptan see full prescribing information from innovator Rizact Monograph, Rizact MSDS, Rizact FDA label

FAQ

What is Rizact used for?

Rizact is used to treat acute migraine headaches in adults and children 6 years of age and older. It is not used to prevent migraine headaches and is not used for cluster headaches. Rizact works in the brain to relieve the pain from migraine headaches.

How does Rizact work?

Rizact works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and blocking the release of certain natural substances that cause pain, nausea, and other symptoms of migraine.

How safe is Rizact?

Rizact can commonly cause chest,jaw,neck tightness, pain, or pressure that is usually not serious. However, these side effects are like symptoms of a heart attack, which may include chest,jaw,left arm pain, shortness of breath, or unusual sweating.

What are the common side effects of Rizact?

Common side effects of Rizact are include:

  • drowsiness
  • dizziness
  • tiredness
  • upset stomach
  • vomiting
  • diarrhea
  • muscle pain or cramps
  • tremors
  • flushing (feeling of warmth)
  • dry mouth

Is Rizact safe during pregnancy?

There is insufficient data to draw conclusions about drug-associated risk for major birth defects and miscarriage; animal studies do not indicate harmful effects at dose levels that exceed therapeutic dose levels with respect to the development of the embryo or fetus, or the course of gestation, parturition and post-natal development.

Is Rizact safe during breastfeeding?

Infant risk should be minimized by avoiding breastfeeding for 24 hours after administration of this drug.There are no data on the effects of this drug on the breastfed infant or its effects on milk production.

Can I drink alcohol with Rizact?

Drinking alcoholic beverages can make headaches worse or cause new headaches to occur. People who suffer from severe headaches should probably avoid alcoholic beverages, especially during a headache.

Can I drive after taking Rizact?

As long as you are feeling dizzy or drowsy, do not drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.

How quickly does Rizact work?

Take 1 tablet (10 mg) at the start of the migraine attack. Rizact should work within 30 minutes. If your migraine improves but then comes back, wait at least 2 hours before taking another tablet (10 mg). Do not take more than 3 tablets (30 mg) in 24 hours.

Does Rizact help with anxiety?

Rizact is good for treating depression and anxiety, but it can cause more withdrawal symptoms if you stop suddenly compared to other antidepressants.

Does Rizact make I gain weight?

While it's true that you may notice some weight gain, the benefits of relieving yourself of migraine pain are stronger. Some users may not see any change in weight, and some may even lose weight.

Is Rizact bad for my heart?

Rizact should not be used by people with heart or blood vessel disease.

Can Rizact cause a stroke?

Rizact may increase your risk of having abnormal heart rhythm, heart attack, angina, or stroke.

Can Rizact make your headache worse?

Using Rizact too often can lead to worsened headaches and can cause your migraines to occur more often.

Who should not take Rizact?

You should not use this medicine if you have uncontrolled high blood pressure, heart problems, a history of heart attack or stroke, or circulation problems that cause a lack of blood supply within the body. Do not take Rizact within 24 hours before or after using another migraine headache medicine.

Can a diabetic take Rizact?

Rizact should not be used by people with heart or blood vessel disease.

What happens if I miss a dose?

Rizact is used as needed, it does not have a daily dosing schedule. Call your doctor promptly if your symptoms do not improve after using Rizact.

What happens if I take too much Rizact?

Using too much Rizact may increase the chance of side effects. Do not use this medicine for a headache that is not a migraine headache.

Is Rizact a blood thinner?

Rizact is a headache medicine that narrows the blood vessels around the brain.

Is Rizact a painkiller?

Rizact is not an ordinary pain reliever. It will not relieve any kind of pain other than migraine headaches.

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*** Taking medicines without doctor's advice can cause long-term problems.
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